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1. 发明授权

US06423689B1 Peptidyl calcium channel blockers 失效
标题翻译：肽基钙通道阻滞剂
公开(公告)号：US06423689B1
公开(公告)日：2002-07-23
申请号：US09212785
申请日：1998-12-16
申请人： Richard John Booth , Louis Brogley , Wayne Livingston Cody , David Thomas Connor , Harriet Wall Hamilton , John Xiaoqiang He , Lain-Yen Hu , Leonard Joseph Lescosky , Thomas Charles Malone , Laszlo Nadasdi , Michael Francis Rafferty , Bruce David Roth , Diego F. Silva , Yuntao Song , Balazs G. Szoke , Laszlo Urge
发明人： Richard John Booth , Louis Brogley , Wayne Livingston Cody , David Thomas Connor , Harriet Wall Hamilton , John Xiaoqiang He , Lain-Yen Hu , Leonard Joseph Lescosky , Thomas Charles Malone , Laszlo Nadasdi , Michael Francis Rafferty , Bruce David Roth , Diego F. Silva , Yuntao Song , Balazs G. Szoke , Laszlo Urge
IPC分类号： A61K3805
CPC分类号： C07K5/06008 , A61K38/00
摘要： The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
摘要翻译：本发明提供了阻断下文所示的式I的钙通道的化合物。本发明还提供了使用式I化合物治疗中风，脑缺血，头部创伤或癫痫的方法以及含有下列化合物的药物组合物：一级方程式

2. 发明授权

US6117841A Substituted peptidylamine calcium channel blockers 失效
标题翻译：取代的肽基胺钙通道阻滞剂
公开(公告)号：US6117841A
公开(公告)日：2000-09-12
申请号：US230229
申请日：1999-01-19
申请人： Lain-Yen Hu , Thomas Charles Malone , Laszlo Nadasdi , Michael Francis Rafferty , Todd Robert Ryder , Diego F. Silva , Yuntao Song , Balazs G. Szoke , Laszlo Urge
发明人： Lain-Yen Hu , Thomas Charles Malone , Laszlo Nadasdi , Michael Francis Rafferty , Todd Robert Ryder , Diego F. Silva , Yuntao Song , Balazs G. Szoke , Laszlo Urge
IPC分类号： A61K38/00 , C07C237/12 , C07C237/14 , C07C237/22 , C07D295/13 , C07K5/06 , A61K38/05 , C07K16/00
CPC分类号： C07D295/13 , C07C237/12 , C07C237/14 , C07C237/22 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06191 , A61K38/00
摘要： The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
摘要翻译： PCT No.PCT / US98 / 10838 Sec。 371日期1999年1月19日 102（e）1999年1月19日PCT PCT 1998年5月28日PCT公布。公开号WO98 / 54123 日期1998年12月3日本发明提供了封闭下述通式I的钙通道的化合物。本发明还提供使用式I化合物治疗中风，脑缺血，头部创伤或癫痫的方法以及含有式I化合物的药物组合物。

3. 发明授权

US06458781B1 Substituted diarylalkyl amides as calcium channel antagonists 失效
标题翻译：取代的二芳基烷基酰胺作为钙通道拮抗剂
公开(公告)号：US06458781B1
公开(公告)日：2002-10-01
申请号：US09403579
申请日：1999-10-25
申请人： David Thomas Connor , Lain-Yen Hu , Thomas Charles Malone , Michael Francis Rafferty , Bruce David Roth , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
发明人： David Thomas Connor , Lain-Yen Hu , Thomas Charles Malone , Michael Francis Rafferty , Bruce David Roth , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
IPC分类号： C07D29520
CPC分类号： C07D295/215 , C07C211/29 , C07C237/06 , C07C237/14 , C07C237/16 , C07C271/22 , C07C2601/14 , C07C2603/18 , C07D209/34 , C07D211/58 , C07D231/56 , C07D295/15 , C07D295/185
摘要： The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.
摘要翻译：本发明提供了阻断钙通道并具有式I的化合物：本发明还提供含有式I化合物的药物组合物及其用于治疗中风，脑缺血，头部创伤和癫痫的方法。

4. 发明授权

US06469038B1 Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers 失效
标题翻译：杂芳基烷基α取代肽基胺钙通道阻断剂
公开(公告)号：US06469038B1
公开(公告)日：2002-10-22
申请号：US09663603
申请日：2000-09-18
申请人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
发明人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
IPC分类号： A61K31425
CPC分类号： C07D213/56 , C07D277/30
摘要： The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
摘要翻译：本发明提供了阻断下文所示的式I的钙通道的化合物。本发明还提供了使用式I化合物治疗中风，脑缺血，头部外伤，哮喘，肌萎缩性侧索硬化或癫痫的药物的方法以及药物含有式I化合物的组合物。

5. 发明授权

US6166052A Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers 失效
公开(公告)号：US6166052A
公开(公告)日：2000-12-26
申请号：US264193
申请日：1999-03-08
申请人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
发明人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
IPC分类号： C07D213/56 , C07D277/30 , C07D213/30 , A61K31/44
CPC分类号： C07D213/56 , C07D277/30
摘要： The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.

6. 发明授权

US06989448B2 Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers 失效
公开(公告)号：US06989448B2
公开(公告)日：2006-01-24
申请号：US10254416
申请日：2002-09-25
申请人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
发明人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
IPC分类号： C07D401/00 , C07D211/08 , A61K31/445 , A61K31/47
CPC分类号： C07D213/56 , C07D277/30
摘要： The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.

7. 发明授权

US06180677B2 Tyrosine-derived compounds as calcium channel antagonists 失效
标题翻译：酪氨酸衍生化合物作为钙通道拮抗剂
公开(公告)号：US06180677B2
公开(公告)日：2001-01-30
申请号：US09381938
申请日：1999-09-27
申请人： Michael Francis Rafferty , Yuntao Song
发明人： Michael Francis Rafferty , Yuntao Song
IPC分类号： A61K3803
CPC分类号： A61K31/4453 , A61K31/137 , A61K31/165 , A61K31/195
摘要： The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.
摘要翻译：本发明提供了阻断钙通道并具有式I的化合物及其药学上可接受的盐，酯和前药，其中R 1和R 2独立地为H，苯基环戊基羰基，C 1 -C 7烷基，环己基甲基，苄基，C 1 -C 5烷基苄基或C 1 -C 5烷氧基苄基，A是-C（O） - 或-CH 2 - ; R 3是H或-CH 3; R 4是C 1 -C 4烷基或哌啶-1-基乙基; R 5是苯基 - （CH 2） C 1 -C 4烷基苯基 - （CH 2）n - 或卤代苯基 - （CH 2）n - 并且n为1或2.本发明还提供了含有式I化合物的药物组合物及其用于治疗中风，脑缺血，头部创伤和癫痫的方法。

8. 发明授权

US06362174B1 Reduced dipeptide analogues as calcium channel antagonitsts 失效
标题翻译：还原二肽类似物作为钙通道拮抗剂
公开(公告)号：US06362174B1
公开(公告)日：2002-03-26
申请号：US09925947
申请日：2001-08-09
申请人： Michael Francis Rafferty , Yuntao Song
发明人： Michael Francis Rafferty , Yuntao Song
IPC分类号： A61K31195
CPC分类号： C07D295/215 , C07C237/20 , C07D295/13
摘要： The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The novel compounds provided by this invention have the Formula I: wherein R1 is H or methyl, R2 is H, azepanylcarbonyl, C1-C7 alkyl, —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo, R3 is C1-C5 alkyl, X is —NR4R5 or —OR7, R4 and R5 are independently H, C1-C5 alkyl, or R4 and R5 together with the nitrogen to which they are both bound form: R6 is —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo, A and B are independently —CO— or —CH2—, provided that A and B are not both —CO—, R7 is C1-C5 alkyl, Z is —CH2—, —O—, —S—, or —N(R8)—, R8 is H or C1-C6 alkyl, and n is 1 or 2.
摘要翻译：本发明提供新型的N型钙通道阻滞剂，包含它们的组合物及其使用方法。本发明的化合物可用于治疗中风，脑缺血，疼痛，癫痫和头部创伤。本发明提供的新化合物具有式I：其中R 1是H或甲基，R 2是H，氮杂环庚烷基羰基，C 1 -C 7烷基， - （CH 2）n - 苯基，其中苯基是未取代的或被C 1 -C 4烷基， C 1 -C 4烷氧基或卤素，R 3是C 1 -C 5烷基，X是-NR 4 R 5或-OR 7，R 4和R 5独立地是H，C 1 -C 5烷基或R 4和R 5与它们所连接的氮一起形成： R 6是 - （CH 2）n - 苯基，其中苯基是未取代的或被C 1 -C 4烷基，C 1 -C 4烷氧基或卤素取代，A和B独立地是-CO-或-CH 2 - ，条件是A和B是不是-CO-，R7是C1-C5烷基，Z是-CH2-，-O - ， - S-或-N（R8） - ，R8是H或C1-C6烷基，并且n是1或2。

9. 发明授权

US06316440B1 Reduced dipeptide analogues as calcium channel antagonists 失效
标题翻译：减少二肽类似物作为钙通道拮抗剂
公开(公告)号：US06316440B1
公开(公告)日：2001-11-13
申请号：US09381983
申请日：1999-12-27
申请人： Michael Francis Rafferty , Yuntao Song
发明人： Michael Francis Rafferty , Yuntao Song
IPC分类号： C07D29520
CPC分类号： C07D295/215 , C07C237/20 , C07D295/13
摘要： The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The novel compounds provided by this invention have Formula (1), wherein R1 is H or methyl; R2 is H, azepanylcarbonyl, C1-C7 alkyl, —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo; R3 is C1-C5 alkyl; X is —NR4R5 or —OR7; R4 and R5 are independently H, C1-C5 alkyl; or R4 and R5 together with the nitrogen to which they are both bound form formulae (a); (b); (c); (d) or (e); R6 is —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo; A and B are independently —CO— or —CH2—, provided that A and B are not both —CO—; R7 is C1-C5 alkyl; Z is —CH2—, —O—, —S—, or —N(R8)—; R8 is H or C1-C6 alkyl; and n is 1 or 2.
摘要翻译：本发明提供新型的N型钙通道阻滞剂，包含它们的组合物及其使用方法。本发明的化合物可用于治疗中风，脑缺血，疼痛，癫痫和头部创伤。本发明提供的新化合物具有式（1），其中R 1是H或甲基; R 2是H，氮杂环庚基羰基，C 1 -C 7烷基， - （CH 2）n - 苯基，其中苯基是未取代的或被C 1 -C 4烷基，C 1 -C 4烷氧基或卤素取代; R3是C1-C5烷基; X是-NR 4 R 5或-OR 7; R4和R5独立地是H，C1-C5烷基; 或R 4和R 5与它们所连接的氮一起形成式（a）; （b）; （C）; （d）或（e）; R 6是 - （CH 2）n - 苯基，其中苯基是未取代的或被C 1 -C 4烷基，C 1 -C 4烷氧基或卤素取代; A和B独立地为-CO-或-CH2-，条件是A和B不同时为-CO-; R7是C1-C5烷基; Z是-CH 2 - ， - O - ， - S-或-N（R 8） - 。 R8是H或C1-C6烷基; n为1或2。

10. 发明授权

US06323243B1 Tyrosine-derived compounds as calcium channel antagonists 失效
标题翻译：酪氨酸衍生化合物作为钙通道拮抗剂
公开(公告)号：US06323243B1
公开(公告)日：2001-11-27
申请号：US09694921
申请日：2000-10-24
申请人： Michael Francis Rafferty , Yuntao Song
发明人： Michael Francis Rafferty , Yuntao Song
IPC分类号： A61K31132
CPC分类号： C07D295/13 , C07C237/20 , C07C237/22 , C07C2601/08
摘要： The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.
摘要翻译：本发明提供了阻断钙通道并具有式I的化合物及其药学上可接受的盐，酯和前药，其中R 1和R 2独立地为H，苯基环戊基羰基，C 1 -C 7烷基，环己基甲基，苄基，C 1 -C 5烷基苄基或C 1 -C 5烷氧基苄基，A是-C（O） - 或-CH 2 - ; R 3是H或-CH 3; R 4是C 1 -C 4烷基或哌啶-1-基乙基; R 5是苯基 - （CH 2） C 1 -C 4烷基苯基 - （CH 2）n - 或卤代苯基 - （CH 2）n - andn为1或2.本发明还提供含有式I化合物的药物组合物及其用于治疗中风，脑缺血，头部创伤和癫痫的方法。

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